FR 139317
Discontinued Product
Chemical Name: N-[N-[N-[(Hexahydro-1H-azepin-1-yl)carbonyl]-L-leucyl]-1-methyl-D-tryptophyl]-3-(2-pyridinyl)-D-alanine
Purity: ≥99%
Biological Activity
FR 139317 is a highly potent and selective ETA endothelin receptor antagonist (Ki values are 1 nM and 7.3 μM at ETA and ETB subtypes respectively). Active in vivo.Technical Data
The technical data provided above is for guidance only.
For batch specific data refer to the Certificate of Analysis.
Tocris products are intended for laboratory research use only, unless stated otherwise.
Background References
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High-throughput genotoxicity assay identifies antioxidants as inducers of DNA damage response and cell death.
Fox JT, Sakamuru S, Huang R
Proc. Natl. Acad. Sci. U.S.A., 2012;109(14):5423-8. -
Subtype selectivity of a novel endothelin antagonist, FR139317, for the two endothelin receptors in transfected Chinese hamster ovary cells.
Aramori et al.
Mol.Pharmacol., 1993;43:127 -
Pharmacological profile of FR139317, a novel, potent endothelin ETA receptor antagonist.
Sogabe et al.
J.Pharmacol.Exp.Ther., 1993;264:1040 -
Role of endothelin ETA- and ETB-receptors in haemodynamic compensation following haemorrhage in anaesthetized rats.
Palacios et al.
Br.J.Pharmacol., 2002;135:876 -
Endothelins: molecular biology, biochemistry, pharmacology, physiology, and pathophysiology.
Rubanyi and Polokoff
Pharmacol.Rev., 1994;46:325
Product Datasheets
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Citation for FR 139317
The citations listed below are publications that use Tocris products. Selected citations for FR 139317 include:
1 Citation: Showing 1 - 1
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Early and late contributions of glutamate and CGRP to mechanical sensitization by endothelin-1.
Authors: Khodorova Et al.
J Pain 2009;10:740
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